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Pharmacology > Test #5 Pain > Flashcards

Test #5 Pain Flashcards

1
Q

What is the prototype drug for steroidal anti-inflammatory drugs

A

Corticosterone

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2
Q

Where does the corticosteroid work in order to block the pain preception?

A

It inhibits the PLA2 which stops the entire cascade which inhibits prostaglandin and leukotriene synthesis

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3
Q

What are some SE from the treatment with steroids?

A

immunosuppression, adrenal insufficiency upon withdrawal, and fever

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4
Q

What is one major SE when on steroids because we are inhibiting the prostaglandin production?

A

Stomach ulcers because we are inhibiting prostaglandins which usually protect the lining of the stomach.

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5
Q

Where exactly do non-steroid anti-inflammatory drugs work?

A

They work by inhibiting COX1 and COX2 which block nociepotor sensitization and they also reduce leukocyte invasion

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6
Q

what is the prototype drug for non-steroid anti-inflammatory drugs?

A

ibuprofen

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7
Q

What is a SE from non-steroid anti-inflammatory drugs? They are weak acids so must take with food or water to prevent ulcers

A

GI upset - bc COX1 normally protects the lining of the stomach

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8
Q

WhAT non-steroid anti-inflammatory drug HAS A REVERSIBLE inhibition of platelet aggregation and in an injectable form that resembles morphine

A

Ketorolac

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9
Q

What are three COX2 inhibitors that have less GI SE because they don’t inhibit COX1?

A

Celeboxib - Celebrex
Robecoxib - Vioxx
Valdecoxib

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10
Q

What are three non-steroid anti-inflammatory drugs that are used to treat Rheumatoid Arthritis (chronic inflam. pain?

A

Diclofenac
Indomethacin
Piroxicam

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11
Q

What are three non-steroid anti-inflammatory drugs used to treat Osteoarthrosis? (phasic inflm pain)

A

Diclofenac
ibuprofen
ketoprofen

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12
Q

What are 4 non-steroid anti-inflammatory drugs to treat Post-op pain or acute pain

A

Diclofenac
ibuprofen
ketoprofen
Flurbiprofen

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13
Q

What are three non-steroid anti-inflammatory drugs to treat HE

A

Naproxen
ibuprofen
ketoprofen

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14
Q

What is one drug that is NOT an NSAID but is used for pain

A

Acetaminophen

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15
Q

What is the main action of acetaminophen?

A

On the CNS - NOT the site of the pain

you need a very high dose (lethal) for inhibit COX

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16
Q

Where is acetaminophen metabolized? and where is it excreted?

A

metabolized in the liver (p450) and excreted by the kidneys - retarded in the elderly and liver disease patients

17
Q

What drug is used for an OD of acetaminophen? you must take within 4 hours to protect liver/prevent damage.

A

N-acetylcysteine

This increases glutathione production - a protective hormone in the liver

18
Q

What are three indications for the use of acetaminophen?

A

HE - some forms (not migraines)
Fever - in kids esp)
Osteroarthritis - its a mechanical disease - not inflammatory

19
Q

What is the prototype drug for opioids? and what receptor does it work on and what is that receptors NT?

A

Morphine —>mu receptors —–> endorphins

20
Q

Name each of the primary NT for each of the receptors.
Mu
Kappa
Delta

A

mu - endorphins

Kappa - dynorphins

Delta - enkephalins

21
Q

What is the #1 universal effect of morphine? everyone gets it? you NEVER develop a tolerance to

and what is another one you never develop a tolerance to?

A

2 - you don’t develop a tolerance to constipation

Constipation!!

Mitosis - pin-point pupils

22
Q

What are three WD symptoms of morphine?

A

hyperalgesia, goose flesh, and Dilated pupils

23
Q

What is responsible for the metabolism of morphine? the active form—and is 100x more potent and responsible for most of the effects?

A

Morphine -3B-glucuronide

24
Q

What drug is about 1/10th the potency of morphine and 5-7% of pt don’t possess the enzyme for the drug to work (CYP450 2D6)

A

Codeine

25
Q

Codeine is a pro-drug so what enzyme do you need in-order to convert this drug into morphine so it can work?

A

CYP450 - 2D6

26
Q

What drug is the same as morphine so its 10x more potent than Codeine? it is also metabolized by the same enzyme (CYP450 - 2D6)

A

Oxycodone

controlled release formula - OxyContin)

27
Q

What drug is just like oxycodone but is given with acetaminophen to get better analgesia at a lower dose?

A

Hydrocodone

28
Q

What drug crosses the BBB, 2-4x more potent than morphine, but has the same efficacy and SE just quicker

A

Heroin - mu receptor

29
Q

What drug is 8-10x more potent than morphine. 4hrs duration and is available as a suppository

A

Hydromorphone (Dilaudid)

also Oxymorphone (Numorphan)

30
Q

What drug is synthetic form of morphine that’s 4hr duration, decreases sm muscle spasms (good for post surgery) no mitosis.

A

Meperidine

Normaperidine is a toxic metabolite that can build up and cause seizures

31
Q

What drug is synthetic form of morphine that is 100x potent, fast onset, short duration < 5 min so must be on continuous infusion. or a lolly pop

A

Fentanyl

32
Q

What drug is synthetic form of morphine but is 4x more potent orally. 24hr t1/2,
Used to tx narcotic dependence

A

Methadone

33
Q

What is the main opioid antagonist? it has a 99% first pass effect so give it IV and short t1/2 so give it often

A

Naloxone - Narcan

34
Q

What drug is an antagonist at Mu and an agonist at Kappa and Delta. Naloxone was added so it has no effect and was kept on the market

A

Pentazocine - Talwin NX

35
Q

What drug is an antagonist at Mu and an agonist at Kappa. Is a nasal spray and is 5x more potent in women than men bc of the hormone receptor is bind to

A

Butorphonal - Stadol

36
Q

What drug is an antagonist at Mu and an agonist at Kappa. Dysphoria at high doses, common in ambulances so they won’t steal the morphine

A

Nalbuphine

37
Q

What drug is a partial agonist at Mu and at Kappa3

Antagonist at Kappa1. Used by ex-drug abusers

A

Buprenorphine

38
Q

What drug is an agonist at Mu and Delta.
A NE and 5-HT reuptake blocker (antidepressant)

Which these two action are synergistic for analgesia - they feel good!!!

A

Tramadol

Pharmacology (12 decks)

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